Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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FIG. 14.11. Coupling efficiency of cDTPA to rituximab TABLE 14.3. REACTION TIME OF DTPA RITUXIMAB Reaction time (min) 1 3 5 7 10 20 60 120 150 Efficiency (%) 99.5 99.5 99.6 99.7 99.8 99.8 99.8 99.8 99.8 Biodistribution of 90 Y DTPA rituximab was investigated in normal mice. After tracer injection in the tail vein, mice were sacrificed at designated time intervals, and organs were removed and counted. The percentage of injected dose per gram of tissue was calculated as shown in Table 14.4. Uptake in the bone was high, even after 2 d of injection. 276
FIG. 14.12. ITLC of 90 Y rituximab. TABLE 14.4. BIODISTRIBUTION OF 90 Y DTPA RITUXIMAB IN NORMAL MICE (%ID/G ± SD) (N = 5) Tissue 1 h 6 h 24 h 72 h 120 h Liver 0.72 ± 0.14 4.45 ± 1.15 5.31 ± 0.76 4.23 ± 1.81 6.22 ± 3.17 Spleen 0.09 ± 0.04 0.24 ± 0.23 0.34 ± 0.12 0.22 ± 0.07 0.30 ± 0.16 Kidneys 0.51 ± 0.17 2.66 ± 1.40 1.95 ± 0.72 1.26 ± 0.56 1.37 ± 0.75 Lungs 0.17 ± 0.02 0.70 ± 0.06 1.75 ± 1.15 0.41 ± 0.20 1.93 ± 2.47 Heart 0.25 ± 0.18 0.40 ± 0.13 0.43 ± 0.07 0.23 ± 0.06 1.27 ± 1.60 Blood 3.20 ± 1.09 13.59 ± 1.08 15.16 ± 2.86 9.56 ± 3.61 3.01 ± 1.37 Stomach 0.66 ± 0.15 0.58 ± 0.08 1.08 ± 0.18 1.27 ± 0.27 3.19 ± 0.54 Bone 4.68 ± 0.79 6.64 ± 2.32 23.92 ± 7.93 38.37 ± 7.68 29.52 ± 9.17 Muscle 4.23 ± 1.62 8.40 ± 3.22 12.86 ± 3.58 9.93 ± 3.15 7.63 ± 2.48 277
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IAEA RADIOISOTOPES AND RADIOPHARMAC
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YTTRIUM-90 AND RHENIUM-188 RADIOPHA
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IAEA RADIOISOTOPES AND RADIOPHARMAC
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FOREWORD The IAEA helps to promote
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CONTENTS CHAPTER 1. INTRODUCTION ..
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7.4. Discussion ...................
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CHAPTER 12. DEVELOPMENT OF 90 Sr/ 9
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Chapter 1 INTRODUCTION 1.1. BACKGRO
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devices were designed to improve th
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etention of the antibody’s target
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Binding affinity of these derivativ
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Chapter 2 FUNDAMENTAL CONCEPTS IN R
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A special characteristic of radioph
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β particles emitted by 90 Y. Numer
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2.3.1. Exploitation of certain meta
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2.3.3. Antibodies The high specific
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cell cultures, presents one example
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Another very promising form of radi
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destructive processes within the jo
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esearch efforts, since then. Howeve
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[2.18] HAMILTON, J.G., The metaboli
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[2.52] GOLDENBERG, D.M., et al., Mu
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Chapter 3 DEVELOPMENT OF RADIOPHARM
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FIG. 3.3. Elution efficiencies for
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FIG. 3.5. Electrodeposition of yttr
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The results of the experiments of r
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TABLE 3.3. RESULTS FOR 90 Sr/ 90 Y
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FIG. 3.11. Elution yield of a 90 Sr
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According to Fig. 3.12, there is a
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eagent (Sigma). The mean recovery o
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FIG. 3.18. Variation of RCP (%) of
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(20 and 30 min) and volume of 188 R
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FIG. 3.24. Variation of labelling y
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(c) Clodronate: 20 mg of clodronate
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Chapter 4 EVALUATION OF THE 90 Sr/
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Kamadhenu consists of five main com
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Quality control of radiolabelling w
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The electrochemical deposition of 9
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FIG. 4.5. Typical pattern of the wh
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FIG. 4.6. Elution profile from the
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FIG. 4.8. CD20 recognition in Ramos
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4.5. RECOMMENDATIONS AND FUTURE WOR
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adioiodine labelled anti-NCAM antib
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FIG. 5.1. Comparison of biodistribu
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FIG. 5.3. Three step strategy. Biot
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TABLE 5.1. THREE STEP PRETARGETING:
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5.1.4. Therapeutic experiments with
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5.1.4.4. Conclusion The radioiodine
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control procedure for detection of
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6.1.3. Recovery of doped 85/89 Sr 2
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6.2. PREPARATION AND BIOEVALUATION
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(a) (b) (c) FIG. 6.5. PD-10 column
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FIG. 6.7. SDS PAGE pattern of ritux
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FIG. 6.10. HPLC pattern of pure 90
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FIG. 6.13. Cell binding studies wit
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6.2.1.6. Conclusion The procedure f
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FIG. 6.17. Elution profile of 90 Y
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form NADH, which, in turn, causes t
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FIG. 6.19. In vivo distribution pat
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ACKNOWLEDGEMENTS The authors of thi
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Chapter 7 DEVELOPMENT OF THERAPEUTI
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the residual breast tissue becoming
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7.2.5.2. Automatic procedure The la
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FIG. 7.2. RCP values of 90 Y r-BHD
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FIG. 7.3. Pyrogen test shows result
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to avidin at the 1:4 avidin:r-BHD m
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[7.9] SU, F.M., GUSTAVSON, L.M., AX
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8.1. INTRODUCTION In past years, th
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(a) FIG. 8.1. (a) Schematic illustr
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Preliminary synthesis of the biotin
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(a) (b) FIG. 8.4. (a) PEGylated and
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TABLE 8.2. BIODISTRIBUTION IN RATS
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A specific binding to avidin was ev
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[8.13] BOSCHI, A., DUATTI, A., UCCE
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90 Y solution obtained from a 90 Sr
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From each fraction, a ~1 g aliquot
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FIG. 9.2. Relationship between 90 S
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with 188 Re obtained from the 188 W
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9.3.2. Labelling of DPA ale DPA ale
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FIG. 9.8. TLC radiochromatogram of
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(-) 188 Re(CO) 3 (+) (-) 99m Tc(CO)
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the HSA solution containing sodium
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TABLE 9.3. RESULTS OF 99m Tc LABELL
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9.4.4. Yttrium-90 and 177 Lu labell
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FIG. 9.14. In vitro stability of 90
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(a) (b) (c) (d) (e) (f) (g) (h) (i)
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TABLE 9.8. YTTRIUM-90 CITRATE COLLO
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(a) (b) FIG. 9.17. Grain size distr
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TABLE 9.10. BIODISTRIBUTION AFTER A
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FIG. 9.19. Structure of DOTA biotin
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[9.8] WESTERA, G., GADZE, A., HORST
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Chapter 10 DEVELOPMENT, PREPARATION
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acidic pH) and the vial heated for
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10.2.2.1. Materials and methods (a)
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Using a semiquantitative method, th
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FIG. 10.3. Whole body, SPECT and ta
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TABLE 10.4. ORGAN DISTRIBUTION STUD
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was assessed by measuring the relea
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—— Biological studies: The whol
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or liver) (see Fig. 10.7). The resu
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(b) Results and discussion Healthy
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and the pellet (particles of HA lab
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FIG. 10.11. Organ distribution stud
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The procedure was as follows: —
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TABLE 10.5. INFLUENCE OF CHEMICAL I
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analysed using ICP OES was within t
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suggested for separation of pure 86
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adionuclidic purity of the 90 Y sol
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FIG. 10.16. (a) Strontium-90/yttriu
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[10.5] DJOKIĆ, D.J., JANKOVIĆ, D.
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Yttrium-90 is one of the radionucli
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(a) (b) (c) The generator was prepa
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—— Development of EPC: The EPC
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FIG. 11.4. Elution curve of 90 Sr e
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11.4. YTTRIUM-90 MAbs The use of th
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FIG. 11.6. RCP measured using ITLC
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FIG. 11.9. Biodistribution of 90 Y
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11.5. YTTRIUM-90 EDTMP Bone metasta
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FIG. 11.14. Electrophoresis of 90 Y
Page 239 and 240: FIG. 11.15. Particle size distribut
Page 241 and 242: 11.7. CONCLUSION During this CRP, a
Page 243 and 244: Chapter 12 DEVELOPMENT OF 90 Sr/ 90
Page 245 and 246: 12.1.1.4. Acid vapour trap and radi
Page 247 and 248: 12.1.8. Yttrium-90 peptide labellin
Page 249 and 250: (a) FIG. 12.3. Yttrium-90 elution p
Page 251 and 252: FIG. 12.6. HPLC of 90 Y DOTATATE. 1
Page 253 and 254: Chapter 13 BIFUNCTIONAL BISPHOSPHON
Page 255 and 256: latter requirement [13.10]. When th
Page 257 and 258: whether the organometallic core sel
Page 259 and 260: The fate of a targeted imaging prob
Page 261 and 262: FIG. 13.7. SPECT/CT images showing
Page 263 and 264: FIG. 13.9. TLC SG analyses of [ 188
Page 265 and 266: FIG. 13.11. Stability study (toward
Page 267 and 268: Ex vivo biodistribution studies at
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Page 271 and 272: FIG. 13.19. Absolute uptake of 99m
Page 273 and 274: [13.2] ZHANG, S., GANGAL, G., ULUDA
Page 275 and 276: [13.31] DE ROSALES, R.T.M., et al.,
Page 277 and 278: The activity due to 90 Sr should be
Page 279 and 280: 14.3.1.2. Operation of the 90 Sr/ 9
Page 281 and 282: antibody were taken, to which 90 Y
Page 283 and 284: operation, radiopharmaceutical grad
Page 285 and 286: 14.4.1.3. Operation of the stage II
Page 287 and 288: A typical EPC pattern for a 90 Y pr
Page 289: FIG. 14.10. Decay curve of carrier
Page 293 and 294: FIG. 14.13. Reaction scheme for lab
Page 295 and 296: TABLE 14.6. STABILITY (%) OF 90 Y D
Page 297 and 298: FIG. 14.18. Microsphere albumin siz
Page 299: [14.3] PANDEY, U., DHAMI, P.S., JAG
Page 302 and 303: naphthalene and 1.2 g of 2,5-diphen
Page 304 and 305: A-2.2. Materials The method for sep
Page 306 and 307: out using a Wallac 1411 spectromete
Page 308 and 309: A-5.3. Procedure The technique was
Page 310 and 311: Although acyclic chelators offer ma
Page 312 and 313: (b) (c) and 90 Y colloids, both ser
Page 315: CONTRIBUTORS TO DRAFTING AND REVIEW
Page 318 and 319: INDIA Allied Publishers 1 st Floor,
Page 320: A key requirement for the effective
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Yttrium-90 and Rhenium-188 Radiopharmaceuticals for Radionuclide Therapy

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